AR078495A1 - POLYCLYTIC COMPOUNDS AS ANTAGONISTS OF THE LISOPHOSPHYTIDIC ACID RECEIVER - Google Patents

POLYCLYTIC COMPOUNDS AS ANTAGONISTS OF THE LISOPHOSPHYTIDIC ACID RECEIVER

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Publication number
AR078495A1
AR078495A1 ARP100103584A ARP100103584A AR078495A1 AR 078495 A1 AR078495 A1 AR 078495A1 AR P100103584 A ARP100103584 A AR P100103584A AR P100103584 A ARP100103584 A AR P100103584A AR 078495 A1 AR078495 A1 AR 078495A1
Authority
AR
Argentina
Prior art keywords
substituted
alkyl
unsubstituted
fluoroalkoxy
heteroalkyl
Prior art date
Application number
ARP100103584A
Other languages
Spanish (es)
Inventor
Ryan Clark
Brian Andrew Stearns
Lucy Zhao
Thomas Jon Seiders
Deborah Volkots
Jeannie M Arruda
Original Assignee
Amira Pharmaceuticals Inc
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43128100&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR078495(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amira Pharmaceuticals Inc filed Critical Amira Pharmaceuticals Inc
Publication of AR078495A1 publication Critical patent/AR078495A1/en

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/08—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

También, se describen composiciones farmacéuticas y medicamentos que incluyen los compuestos que se describen en la presente, así como también métodos para la utilizacion de dichos antagonistas, solos y en combinacion con otros compuestos, con el fin de tratar los estados de salud o enfermedades dependientes del LPA o intermediadas por el LPA. Reivindicacion 1: Un compuesto que tiene la estructura la formula (1), o una sal del mismo aceptable desde el punto de vista farmacéutico caracterizado porque, R1 es -CO2RD, -C(=O)NHSO2RE, -C(=O)N(RD)2, -CN, o tetrazolilo; RD es H o alquilo C1-6, RE es alquilo C1-6 o un fenilo substituido o no substituido; L2 está ausente, es -C(=O)-, -N(RD)-, alquileno C1-4 substituido o no substituido, o heteroarileno C1-4 substituido o no substituido, caracterizado porque si L2 es substituido, entonces L2 es substituido con R12, caracterizado porque R12 es F, alquilo C1-4, -OH, o -ORD; el anillo A es un fenilo substituido o no substituido, o heteroarileno C1-5 monocíclico substituido o no substituido, caracterizado porque si el anillo A es substituido, entonces el anillo A es substituido con 1 o 2 de R14; cada R14 se selecciona independientemente de halogeno, -CN, -OH, alquilo C1-4, fluoroalquilo C1-4, fluoroalcoxi C1-4, alcoxi C1-4, y heteroalquilo C1-4; L4 está ausente, o es un alquileno C1-4 substituido o no substituido, caracterizado porque si L4 es substituido entonces L4 es substituido con R13, caracterizado porque R13 es F, alquilo C1-4, -OH, o -ORD; R5 es H o alquilo C1-4; cada RA se selecciona independientemente de halogeno, -CN, -OH, alquilo C1-4, fluoroalquilo C1-4, fluoroalcoxi C1-4, alcoxi C1-4, y heteroalquilo C1-4; cada RB se selecciona independientemente de halogeno, -CN, -OH, alquilo C1-4, fluoroalquilo C1-4, fluoroalcoxi C1-4, alcoxi C1-4 y heteroalquilo C1-4; cada RC se selecciona independientemente de halogeno, -CN, -OH, alquilo C1-4, fluoroalquilo C1-4, fluoroalcoxi C1-4, alcoxi C1-4 y heteroalquilo C1-4, m es 0, 1 o 2; n es 0, 1 o 2; p es 0, 1 o 2; r es 1, 2, 3 o 4.Also, pharmaceutical compositions and medicaments are described which include the compounds described herein, as well as methods for the use of said antagonists, alone and in combination with other compounds, in order to treat health conditions or dependent diseases. of the LPA or intermediated by the LPA. Claim 1: A compound having the structure formula (1), or a pharmaceutically acceptable salt thereof characterized in that, R1 is -CO2RD, -C (= O) NHSO2RE, -C (= O) N (RD) 2, -CN, or tetrazolyl; RD is H or C1-6 alkyl, RE is C1-6 alkyl or a substituted or unsubstituted phenyl; L2 is absent, it is -C (= O) -, -N (RD) -, substituted or unsubstituted C1-4 alkylene, or substituted or unsubstituted C1-4 heteroarylene, characterized in that if L2 is substituted, then L2 is substituted with R12, characterized in that R12 is F, C1-4 alkyl, -OH, or -ORD; ring A is a substituted or unsubstituted phenyl, or substituted or unsubstituted monocyclic C1-5 heteroarylene, characterized in that if ring A is substituted, then ring A is substituted with 1 or 2 of R14; each R14 is independently selected from halogen, -CN, -OH, C1-4 alkyl, C1-4 fluoroalkyl, C1-4 fluoroalkoxy, C1-4 alkoxy, and C1-4 heteroalkyl; L4 is absent, or is a substituted or unsubstituted C1-4 alkylene, characterized in that if L4 is substituted then L4 is substituted with R13, characterized in that R13 is F, C1-4 alkyl, -OH, or -ORD; R5 is H or C1-4 alkyl; each RA is independently selected from halogen, -CN, -OH, C 1-4 alkyl, C 1-4 fluoroalkyl, C 1-4 fluoroalkoxy, C 1-4 alkoxy, and C 1-4 heteroalkyl; each RB is independently selected from halogen, -CN, -OH, C 1-4 alkyl, C 1-4 fluoroalkyl, C 1-4 fluoroalkoxy, C 1-4 alkoxy and C 1-4 heteroalkyl; each RC is independently selected from halogen, -CN, -OH, C1-4 alkyl, C1-4 fluoroalkyl, C1-4 fluoroalkoxy, C1-4 alkoxy and C1-4 heteroalkyl, m is 0, 1 or 2; n is 0, 1 or 2; p is 0, 1 or 2; r is 1, 2, 3 or 4.

ARP100103584A 2009-10-01 2010-10-01 POLYCLYTIC COMPOUNDS AS ANTAGONISTS OF THE LISOPHOSPHYTIDIC ACID RECEIVER AR078495A1 (en)

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US (3) US8778983B2 (en)
EP (2) EP2483269A4 (en)
JP (2) JP2013506680A (en)
KR (1) KR20120097490A (en)
CN (2) CN102770415B (en)
AR (1) AR078495A1 (en)
AU (1) AU2010300594A1 (en)
BR (1) BR112012007102A2 (en)
CA (1) CA2776779A1 (en)
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Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010068775A2 (en) 2008-12-11 2010-06-17 Amira Pharmaceuticals, Inc. Alkyne antagonists of lysophosphatidic acid receptors
GB2466121B (en) 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
GB2470833B (en) 2009-06-03 2011-06-01 Amira Pharmaceuticals Inc Polycyclic antagonists of lysophosphatidic acid receptors
WO2011017350A2 (en) 2009-08-04 2011-02-10 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
CA3240281A1 (en) 2010-06-03 2011-12-08 Pharmacyclics Llc Use of inhibitors of bruton's tyrosine kinase (btk) in the treatment of follicular lymphoma
CN103002896A (en) 2010-06-16 2013-03-27 布鲁斯·钱德勒·梅 Use of levocetirizine and montelukast in the treatment of influenza, common cold and inflammation
WO2012100436A1 (en) 2011-01-30 2012-08-02 Curegenix Inc. Compound as antagonist of lysophosphatidic acid receptor, composition, and use thereof
EP2694496A1 (en) 2011-04-05 2014-02-12 Amira Pharmaceuticals, Inc. 3- or 5 - bi phenyl - 4 - ylisoxazole - based compounds useful for the treatment of fibrosis, pain, cancer and respiratory, allergic, nervous system or cardiovascular disorders
KR101369584B1 (en) 2011-04-19 2014-03-06 일양약품주식회사 Phenyl-isoxazol derivatives and preparation process thereof
US20150164874A1 (en) * 2011-05-25 2015-06-18 Intermune, Inc. Pirfenidone and anti-fibrotic therapy in selected patients
JP5978302B2 (en) * 2011-08-08 2016-08-24 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ (N-Benzimidazol-2-yl) -cyclopropanecarboxamide as a lysophosphatidic acid antagonist
WO2013025733A1 (en) 2011-08-15 2013-02-21 Intermune, Inc. Lysophosphatidic acid receptor antagonists
GB2493914A (en) * 2011-08-19 2013-02-27 Univ Jw Goethe Frankfurt Main Flurbiprofen and related compounds for the treatment of skin diseases
WO2013070879A1 (en) * 2011-11-10 2013-05-16 Bristol-Myers Squibb Company Methods for treating spinal cord injury with lpa receptor antagonists
MX2014006130A (en) 2011-11-22 2015-04-13 Intermune Inc Methods of diagnosing and treating idiopathic pulmonary fibrosis.
WO2013085824A1 (en) * 2011-12-04 2013-06-13 Angion Biomedica Corp. Small molecule anti-fibrotic compounds and uses thereof
KR20150021057A (en) * 2012-06-20 2015-02-27 에프. 호프만-라 로슈 아게 N-alkyltriazole compounds as lpar antagonists
EP2877598A1 (en) 2012-07-24 2015-06-03 Pharmacyclics, Inc. Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk)
JP6176258B2 (en) 2012-12-28 2017-08-09 宇部興産株式会社 Halogen-substituted heterocyclic compounds
CN103965664B (en) * 2013-01-25 2015-07-22 中国石油化工股份有限公司 Carbon black particle dispersing agent, preparation method and application thereof
CA2901421A1 (en) 2013-03-13 2014-10-09 Bruce Chandler May Use of levocetirizine and montelukast in the treatment of autoimmune disorders
CN105517631A (en) 2013-03-13 2016-04-20 炎症反应研究公司 Use of levocetirizine and montelukast in the treatment of traumatic injury
RU2015134422A (en) 2013-03-13 2017-04-18 Инфламматори Респонс Ресёрч, Инк. APPLICATION OF LEVOCYTHIRIZINE AND MONTELUKAST IN THE TREATMENT OF VASCULITIS
DK2988743T3 (en) 2013-03-15 2021-03-01 Epigen Biosciences Inc HETEROCYCLIC COMPOUNDS WHICH MAY BE USED FOR DISEASE TREATMENT
WO2015013579A1 (en) 2013-07-26 2015-01-29 Update Pharma Inc. Compositions to improve the therapeutic benefit of bisantrene
GB201314926D0 (en) * 2013-08-20 2013-10-02 Takeda Pharmaceutical Novel Compounds
US9981942B2 (en) * 2013-12-20 2018-05-29 Laboratorios Del Dr. Esteve S.A. Piperidine derivatives having multimodal activity against pain
JP2017078022A (en) * 2014-02-28 2017-04-27 クミアイ化学工業株式会社 Isoxazole derivative, and agricultural and horticultural plant disease control agent prepared therewith
CA2953472C (en) 2014-06-27 2022-08-02 Ube Industries, Ltd. Halogen-substituted heterocyclic compound salt
JP2017526728A (en) 2014-09-15 2017-09-14 インフラマトリー・レスポンス・リサーチ・インコーポレイテッド Levocetirizine and montelukast in the treatment of inflammation-mediated conditions
AU2015369665A1 (en) * 2014-12-23 2017-06-29 Pharmacyclics Llc BTK inhibitor combinations and dosing regimen
US9729562B2 (en) 2015-03-02 2017-08-08 Harris Corporation Cross-layer correlation in secure cognitive network
CA2988306A1 (en) 2015-06-05 2016-12-08 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of demyelinating diseases
AR108838A1 (en) 2016-06-21 2018-10-03 Bristol Myers Squibb Co CARBAMOYLOXIMETHYL ACID TRIAZOL CYCLOHEXILO AS LPA ANTAGONISTS
CN107840842A (en) * 2016-09-19 2018-03-27 北京天诚医药科技有限公司 Alkynes is for heterocyclic compound, its preparation method and its in application pharmaceutically
WO2018106643A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Heterocyclic azoles for the treatment of demyelinating diseases
WO2018106641A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Pyrazoles for the treatment of demyelinating diseases
WO2018106646A1 (en) 2016-12-06 2018-06-14 Vertex Pharmaceuticals Incorporated Aminotriazoles for the treatment of demyelinating diseases
WO2019041340A1 (en) * 2017-09-04 2019-03-07 Eli Lilly And Company Lysophosphatidic acid receptor 1 (lpar1) inhibitor compounds
US11498904B2 (en) 2017-11-14 2022-11-15 Merck Sharp & Dohme Llc Substituted biaryl compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
TWI815829B (en) 2017-11-14 2023-09-21 美商默沙東有限責任公司 Novel substituted biaryl compounds as indoleamine 2,3-dioxygenase (ido) inhibitors
CN109776351B (en) * 2017-11-15 2021-11-09 江苏优士化学有限公司 Diazoacetic ester continuous synthesis method
WO2019126086A1 (en) 2017-12-19 2019-06-27 Bristol-Myers Squibb Company Cyclohexyl acid isoxazole azines as lpa antagonists
SG11202005703TA (en) 2017-12-19 2020-07-29 Bristol Myers Squibb Co Cyclohexyl acid triazole azoles as lpa antagonists
CN112041302A (en) 2017-12-19 2020-12-04 百时美施贵宝公司 Pyrazole O-linked carbamoylcyclohexanoic acids as LPA antagonists
RS62710B1 (en) 2017-12-19 2022-01-31 Bristol Myers Squibb Co Triazole n-linked carbamoyl cyclohexyl acids as lpa antagonists
EP3728223B1 (en) 2017-12-19 2022-12-28 Bristol-Myers Squibb Company Cyclohexyl acid triazole azines as lpa antagonists
EP3728222B1 (en) 2017-12-19 2023-03-29 Bristol-Myers Squibb Company Cyclohexyl acid pyrazole azines as lpa antagonists
EP3728240B1 (en) 2017-12-19 2022-06-29 Bristol-Myers Squibb Company Isoxazole o-linked carbamoyl cyclohexyl acids as lpa antagonists
JP7256807B2 (en) * 2017-12-19 2023-04-12 ブリストル－マイヤーズ スクイブ カンパニー Cyclohexylate isoxazole azoles as LPA antagonists
EP3727589B1 (en) 2017-12-19 2022-06-29 Bristol-Myers Squibb Company Cyclohexyl acid pyrazole azoles as lpa antagonists
BR112020011953A2 (en) 2017-12-19 2020-11-17 Bristol-Myers Squibb Company pyrazole-linked carbamoyl cyclohexyl acids as lpa antagonists
CN112041304A (en) 2017-12-19 2020-12-04 百时美施贵宝公司 Isoxazole N-linked carbamoylcyclohexanoic acids as LPA antagonists
CN108379275B (en) * 2018-05-29 2020-05-22 中国医学科学院阜外医院 Lysophosphatidic acid, lysophosphatidic acid receptor 3, and use of lysophosphatidic acid receptor 3 agonist
WO2020060915A1 (en) 2018-09-18 2020-03-26 Bristol-Myers Squibb Company Cyclopentyl acids as lpa antagonists
CN114599641A (en) 2019-06-18 2022-06-07 百时美施贵宝公司 Cyclobutylcarboxylic acids as LPA antagonists
WO2020257138A1 (en) 2019-06-18 2020-12-24 Bristol-Myers Squibb Company Isoxazole carboxylic acids as lpa antagonists
CN114728168B (en) 2019-11-15 2024-04-09 吉利德科学公司 Triazole carbamate pyridylsulfonamides as LPA receptor antagonists and their use
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use
JP2023519892A (en) 2020-03-27 2023-05-15 ランドス バイオファーマ インコーポレイテッド PLXDC2 ligand
EP4161936A1 (en) 2020-06-03 2023-04-12 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
TWI838626B (en) 2020-06-03 2024-04-11 美商基利科學股份有限公司 Lpa receptor antagonists and uses thereof
EP4337641A1 (en) 2021-05-11 2024-03-20 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
AU2022405082A1 (en) 2021-12-08 2024-07-11 Gilead Sciences, Inc. Lpa receptor antagonists and uses thereof
AR128613A1 (en) 2022-02-25 2024-05-29 Lhotse Bio Inc COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF CONDITIONS ASSOCIATED WITH THE ACTIVITY OF THE LPA RECEPTOR
CN114907282B (en) * 2022-05-24 2023-08-22 华南理工大学 Method for synthesizing 4-phenyl alkenyl isoxazole derivative

Family Cites Families (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
AU6645998A (en) 1996-12-23 1998-07-17 Du Pont Pharmaceuticals Company Oxygen or sulfur containing heteroaromatics as factor xa inhibitors
JP3237608B2 (en) 1997-04-21 2001-12-10 住友製薬株式会社 Isoxazole derivative
DE60003025T2 (en) 1999-04-02 2004-03-18 Bristol-Myers Squibb Pharma Co. ARYLSULFONYLE AS FACTOR XA INHIBITORS
WO2001060819A1 (en) 2000-02-18 2001-08-23 Kirin Beer Kabushiki Kaisha Novel isoxazole and thiazole compounds and use thereof as drugs
AU4456601A (en) * 2000-03-28 2001-10-08 Nippon Soda Co., Ltd. Oxa(thia)zolidine derivative and anti-inflammatory drug
WO2002000651A2 (en) 2000-06-27 2002-01-03 Bristol-Myers Squibb Pharma Company Factor xa inhibitors
EP1340749A4 (en) 2000-11-17 2007-09-05 Takeda Pharmaceutical Isoxazole derivatives
JP4396808B2 (en) * 2001-02-08 2010-01-13 小野薬品工業株式会社 Urological disease therapeutic agent comprising LPA receptor modulator
US7521192B2 (en) 2001-04-18 2009-04-21 Rigel Pharmaceuticals, Inc. EDG: modulators of lymphocyte activation and migration
EP1415667B1 (en) 2001-07-17 2008-09-03 Ono Pharmaceutical Co., Ltd. Pancreatic juice secretion regulators comprising lpa receptor controller
MY151199A (en) * 2001-11-02 2014-04-30 Rigel Pharmaceuticals Inc Substituted diphenyl heterocycles useful for treating hcv infection
JP4569106B2 (en) * 2001-12-25 2010-10-27 味の素株式会社 Organ fibrosis inhibitor
JP2003261545A (en) 2001-12-28 2003-09-19 Takeda Chem Ind Ltd Neurotrophic factor production/secretion accelerator
US20050113283A1 (en) * 2002-01-18 2005-05-26 David Solow-Cordero Methods of treating conditions associated with an EDG-4 receptor
US20050261298A1 (en) * 2002-01-18 2005-11-24 David Solow-Cordero Methods of treating conditions associated with an Edg-7 receptor
WO2003062392A2 (en) 2002-01-18 2003-07-31 Ceretek Llc Methods of treating conditions associated with an edg receptor
US20050101518A1 (en) * 2002-01-18 2005-05-12 David Solow-Cordero Methods of treating conditions associated with an EDG-2 receptor
JP4547912B2 (en) * 2002-03-05 2010-09-22 小野薬品工業株式会社 8-Azaprostaglandin derivative compound and drug containing the compound as an active ingredient
US20040014662A1 (en) * 2002-05-08 2004-01-22 Per Lindquist Modulation of neural stem cells and neural progenitor cells
CA2484233A1 (en) * 2002-05-13 2003-11-27 Eli Lilly And Company Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
WO2003099765A1 (en) * 2002-05-28 2003-12-04 Ono Pharmaceutical Co., Ltd. β-ALANINE DERIVATIVE AND USE THEREOF
TW200400930A (en) 2002-06-26 2004-01-16 Ono Pharmaceutical Co Therapeutic agent for chronic disease
WO2004031118A1 (en) 2002-10-03 2004-04-15 Ono Pharmaceutical Co., Ltd. Lpa receptor antagonists
US20040171037A1 (en) 2002-11-19 2004-09-02 Jing Li Amplified genes involved in cancer
US20040192739A1 (en) 2003-01-16 2004-09-30 David Solow-Cordero Methods of treating conditions associated with an Edg-2 receptor
US20040167132A1 (en) 2003-01-16 2004-08-26 Geetha Shankar Methods of treating conditions associted with an Edg-2 receptor
US20050065194A1 (en) * 2003-01-16 2005-03-24 Geetha Shankar Methods of treating conditions associated with an Edg-2 receptor
US7135469B2 (en) * 2003-03-18 2006-11-14 Bristol Myers Squibb, Co. Linear chain substituted monocyclic and bicyclic derivatives as factor Xa inhibitors
AU2004229467B2 (en) 2003-04-11 2007-01-25 The University Of Tennessee Research Foundation Lysophosphatidic acid analogs and inhibition of neointima formation
WO2004099164A1 (en) 2003-05-02 2004-11-18 Rigel Pharmaceuticals, Inc. Substituted diphenyl isoxazoles, pyrazoles and oxadiazoles useful for treating hcv infection
SI1638551T1 (en) 2003-05-19 2012-04-30 Irm Llc Immunosuppressant compounds and compositions
JP4692281B2 (en) * 2003-08-05 2011-06-01 味の素株式会社 New azole compounds
JP5048333B2 (en) 2003-10-09 2012-10-17 ユニバーシティ オブ テネシー リサーチ ファウンデーション LPA receptor agonists and antagonists and methods of use
WO2005058790A1 (en) 2003-12-19 2005-06-30 Ono Pharmaceutical Co., Ltd. Compounds having lysophosphatidic acid receptor antagonism and uses thereof
DE10360369A1 (en) 2003-12-22 2005-07-14 Bayer Cropscience Ag amides
WO2005123671A1 (en) * 2004-06-22 2005-12-29 Taisho Pharmaceutical Co., Ltd. Pyrrole derivative
JP2006096712A (en) 2004-09-30 2006-04-13 Senju Pharmaceut Co Ltd Corneal sensitivity improver containing lpa receptor antagonist
CA2610310A1 (en) 2005-06-08 2006-12-14 Novartis Ag Polycyclic oxadiazoles or isoxazoles and their use as s1p receptor ligands
WO2007007588A1 (en) 2005-07-08 2007-01-18 Ono Pharmaceutical Co., Ltd. Compound having cyclic group with planarity as core
CA2619101A1 (en) 2005-08-23 2007-03-01 Irm Llc Immunosuppressant compounds and compositions
CA2643670A1 (en) 2006-02-27 2007-08-30 Sterix Limited Diaryl compounds as non-steroidal inhibitors of 17-beta hydroxysteroid dehydrogenase and/or steroid sulphatase for the treatment of oestrogen-related diseases such as hormone dependent breast cancer
WO2007139946A2 (en) 2006-05-25 2007-12-06 University Of Tennessee Research Foundation Gpcr ligands identified by computational modeling
EP2054424A1 (en) 2006-07-24 2009-05-06 University Of Virginia Patent Foundation Vinyl phosphonate lysophosphatidic acid receptor antagonists
US20080051372A1 (en) 2006-08-24 2008-02-28 The Scripps Research Institute Methods utilizing cell-signaling lysophospholipids
WO2008024979A2 (en) 2006-08-24 2008-02-28 The Scripps Research Institute Methods utilizing cell-signaling lysophospholipids
US20100143381A1 (en) 2007-03-12 2010-06-10 Andrew Tager Lysophosphatidic acid receptor targeting for lung disease
US9163091B2 (en) 2007-05-30 2015-10-20 Lpath, Inc. Compositions and methods for binding lysophosphatidic acid
US20090069288A1 (en) 2007-07-16 2009-03-12 Breinlinger Eric C Novel therapeutic compounds
AU2009243756B2 (en) 2008-05-05 2013-06-27 Sanofi-Aventis Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
JP4933512B2 (en) 2008-10-09 2012-05-16 住友化学株式会社 Light guide plate
WO2010068775A2 (en) 2008-12-11 2010-06-17 Amira Pharmaceuticals, Inc. Alkyne antagonists of lysophosphatidic acid receptors
GB2466121B (en) * 2008-12-15 2010-12-08 Amira Pharmaceuticals Inc Antagonists of lysophosphatidic acid receptors
GB2470833B (en) 2009-06-03 2011-06-01 Amira Pharmaceuticals Inc Polycyclic antagonists of lysophosphatidic acid receptors
WO2011017350A2 (en) 2009-08-04 2011-02-10 Amira Pharmaceuticals, Inc. Compounds as lysophosphatidic acid receptor antagonists
GB2474748B (en) 2009-10-01 2011-10-12 Amira Pharmaceuticals Inc Polycyclic compounds as lysophosphatidic acid receptor antagonists
WO2011041551A1 (en) 2009-10-01 2011-04-07 Intermune, Inc. Therapeutic antiviral peptides
GB2474120B (en) 2009-10-01 2011-12-21 Amira Pharmaceuticals Inc Compounds as Lysophosphatidic acid receptor antagonists
KR101628737B1 (en) * 2010-01-06 2016-06-13 애플 인크. Device, method, and graphical user interface for mapping directions between search results

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